Synthesis and biological evaluation of heterocycle containing adamantane 11β-HSD1 inhibitors

Autor:	William J. Chiou, Jiahong Wang, Jyoti R. Patel, Peer B. Jacobson, Michael E. Brune, J.T. Link, Ravi Kurukulasuriya, Hong Yong, Hing L. Sham, Steven Fung, Katina Monzon, DeAnne Stolarik, Hovis M. Imade, David W A Beno, Vince Yeh
Rok vydání:	2006
Předmět:	medicine.drug_class Adamantane Clinical Biochemistry Drug Evaluation Preclinical Molecular Conformation Pharmaceutical Science Carboxamide In Vitro Techniques Biochemistry Chemical synthesis Cell Line Mice Structure-Activity Relationship chemistry.chemical_compound Heterocyclic Compounds 11-beta-Hydroxysteroid Dehydrogenase Type 2 Amide 11-beta-Hydroxysteroid Dehydrogenase Type 1 Drug Discovery medicine Animals Humans Organic chemistry Enzyme Inhibitors Molecular Biology chemistry.chemical_classification biology Chemistry Organic Chemistry Stereoisomerism Biological activity Enzyme Activation Heterocyclic compound Enzyme inhibitor Microsomes Liver biology.protein Molecular Medicine Selectivity hormones hormone substitutes and hormone antagonists
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 16:5414-5419
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2006.07.055
Popis:	A series of metabolically stable adamantane amide 11beta-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1 potency and HSD2 selectivity and good pharmacokinetic and pharmacodynamic profiles.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::401f7c072da604f9bdd8ef80c7fb5c64 https://doi.org/10.1016/j.bmcl.2006.07.055 Zobrazit plný text záznamu Full Text from ScienceDirect